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Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones

Title
Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones
Authors
Rhee H.-K.Park H.J.Lee S.K.Lee C.-O.Choo H.-Y.P.
Ewha Authors
박혜영이상국
SCOPUS Author ID
박혜영scopus
Issue Date
2007
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 15, no. 4, pp. 1651 - 1658
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Benzofuroquinolinediones (7c and 7d) were synthesized by base-catalyzed condensation of dichloroquinolinediones with phenolic derivatives. Their dialkylaminoalkoxy derivatives (8i-8p) were prepared by reaction with various dialkylaminoalkyl chlorides. The cytotoxicity of the synthesized compounds was evaluated against eight types of human cancer cell lines, and their topoisomerase II inhibition was assessed. In general, the cytotoxicity of benzofuroquinolinediones (8i-8p) was similar or superior to that of doxorubicin and showed more potent inhibitory activity than naphthofurandiones (8a-8h). Also, most of the compounds exhibited excellent topoisomerase II inhibitory activity at a concentration of 5 μM and two compounds, 8d and 8i, showed IC 50 values of 1.19 and 0.68 μM, respectively, and were much more potent than etoposide (IC 50 = 78.4 μM), but similar to doxorubicin (IC 50 = 2.67 μM). However their inhibitory activity on topoisomerase I was lower, and 8d and 8i showed IC 50 values of 42.0 and 64.3 μM, respectively. © 2006.
DOI
10.1016/j.bmc.2006.12.012
Appears in Collections:
약학대학 > 약학과 > Journal papers
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